Effects of K-115 (Ripasudil), a novel ROCK inhibitor, on trabecular meshwork and Schlemms canal endothelial cells

Scientific Reports

Volumn 6, Issue , 2016, Pages

  Kaneko, Yoshio ^a   Ohta, Masayuki ^a   Inoue, Toshihiro ^b   Mizuno, Ken ^a   Isobe, Tomoyuki ^a   Tanabe, Sohei ^a   Tanihara, Hidenobu ^b  

^a KOWA COMPANY LTD   (Japan)

^b KUMAMOTO UNIVERSITY   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

ACTIN; EYE DROPS; ISOQUINOLINE DERIVATIVE; K-115; PROTEIN ZO1; RHO KINASE; SULFONAMIDE;

ANIMAL; ANTAGONISTS AND INHIBITORS; CELL CULTURE; DRUG EFFECTS; ENDOTHELIUM CELL; GLAUCOMA; HAPLORHINI; INTRAOCULAR PRESSURE; JAPAN; MALE; METABOLISM; OCULAR HYPERTENSION; RABBITS AND HARES; TIGHT JUNCTION; TRABECULAR MESHWORK;

ACTINS; ANIMALS; CELLS, CULTURED; ENDOTHELIAL CELLS; GLAUCOMA; HAPLORHINI; INTRAOCULAR PRESSURE; ISOQUINOLINES; JAPAN; MALE; OCULAR HYPERTENSION; OPHTHALMIC SOLUTIONS; RABBITS; RHO-ASSOCIATED KINASES; SULFONAMIDES; TIGHT JUNCTIONS; TRABECULAR MESHWORK; ZONULA OCCLUDENS-1 PROTEIN;

EID: 84955488006     PISSN: None     EISSN: 20452322     Source Type: Journal    
DOI: 10.1038/srep19640     Document Type: Article

References (52)

1. Ishizaki, T. et al. The small GTP-binding protein Rho binds to and activates a 160 kDa Ser/Thr protein kinase homologous to myotonic dystrophy kinase. EMBO. J. 15, 1885-1893 (1996).
2. Shimokawa, H. & Takeshita, A. Rho-kinase is an important therapeutic target in cardiovascular medicine. Arterioscler. Thromb. Vasc. Biol. 25, 1767-1775 (2005).
3. Sagawa, H. et al. A novel ROCK inhibitor, Y-39983, promotes regeneration of crushed axons of retinal ganglion cells into the optic nerve of adult cats. Exp. Neurol. 205, 230-240 (2007).
4. Tan, H. B., Zhong, Y. S., Cheng, Y. & Shen, X. Rho/ROCK pathway and neural regeneration: A potential therapeutic target for central nervous system and optic nerve damage. Int. J. Ophthalmol. 4, 652-657 (2011).
5. Bertrand, J., Winton, M. J., Rodriguez-Hernandez, N., Campenot, R. B. & McKerracher, L. Application of Rho antagonist to neuronal cell bodies promotes neurite growth in compartmented cultures and regeneration of retinal ganglion cell axons in the optic nerve of adult rats. J. Neurosci. 25, 1113-1121 (2005).
6. Stiles, J. M., Kurisetty, V., Mitchell, D. C. & Bryan, B. A. Rho kinase proteins regulate global miRNA expression in endothelial cells. Cancer Genomics Proteomics 10, 251-263 (2013).
7. Nakagawa, O. et al. ROCK-I and ROCK-II, two isoforms of Rho-associated coiled-coil forming protein serine/threonine kinase in mice. FEBS Lett. 392, 189-193 (1996).
8. Fukiage, C., Mizutani, K., Kawamoto, Y., Azuma, M. & Shearer, T. R. Involvement of Phosphorylation of Myosin Phosphatase by ROCK in Trabecular Meshwork and Ciliary Muscle Contraction. Biochem. Biophys. Res. Commun. 288, 296-300 (2001).
9. Waki, M., Yoshida, Y., Oka, T. & Azuma, M. Reduction of intraocular pressure by topical administration of an inhibitor of the Rhoassociated protein kinase. Curr. Eye Res. 22, 470-474 (2001).
10. Tamura, M. et al. Development of specific Rho-kinase inhibitors and their clinical application. Biochim. Biophys. Acta. 1754, 245-252 (2005).
11. Yokota, T. et al. Involvement of the Rho/Rho kinase signaling pathway in platelet-derived growth factor BB-induced vascular endothelial growth factor expression in diabetic rat retina. Jpn. J. Ophthalmol. 51, 424-430 (2007).
12. Arita, R. et al. Rho kinase inhibition by fasudil ameliorates diabetes-induced microvascular damage. Diabetes 58, 215-226 (2009).
13. Hollanders, K. et al. The effect of AMA0428, a novel and potent ROCK inhibitor, in a model of neovascular age-related macular degeneration. Invest. Ophthalmol. Vis. Sci. 56, 1335-1348 (2015).
14. Zandi, S. et al. ROCK-isoform-specific polarization of macrophages associated with age-related macular degeneration. Cell Rep. 10, 1173-1186 (2015).
15. Cho, H. J. & Yoo, J. Rho activation is required for transforming growth factor-beta-induced epithelial-mesenchymal transition in lens epithelial cells. Cell Biol. Int. 31, 1225-1230 (2007).
16. Okumura, N. et al. The new therapeutic concept of using a rho kinase inhibitor for the treatment of corneal endothelial dysfunction. Cornea 30, S54-59 (2011).
17. Zheng, Y. et al. Involvement of rho-kinase pathway in contractile activity of rabbit RPE cells in vivo and in vitro. Invest. Ophthalmol. Vis. Sci. 45, 668-674 (2004).
18. Hirata, A. et al. Y-27632, a Rho-associated protein kinase inhibitor, attenuates neuronal cell death after transient retinal ischemia. Graefes Arch. Clin. Exp. Ophthalmol. 246, 51-59 (2008).
19. Honjo, M. et al. Effects of Rho-Associated Protein Kinase Inhibitor Y-27632 on Intraocular Pressure and Outflow Facility. Invest. Ophthalmol. Vis. Sci. 42, 137-144 (2001).
20. Honjo, M. et al. Effects of protein kinase inhibitor, HA1077, on intraocular pressure and outflow facility in rabbit eyes. Arch. Ophthalmol. 119, 1171-1178 (2001).
21. Quigley, H. A. Open-angle glaucoma. N. Engl. J. Med. 328, 1097-106 (1993).
22. van der Valk, R. et al. Intraocular pressure-lowering effects of all commonly used glaucoma drugs: A meta-analysis of randomized clinical trials. Ophthalmology 112, 1177-1185 (2005).
23. Japanese Ophthalmologic Society, The Japan Glaucoma Society Guidelines for Glaucoma (3rd Edition). Nihon Ganka Gakkai Zasshi. 116, 3-46 (2012). (in Japanese).
24. Nakai, Y. Current status of glaucoma therapy at private practices and a private ophthalmology hospital. Atarashii Ganka (J. Eye) 25, 1581-1585 (2008). (in Japanese).
25. Grierson, I., Jonsson, M. & Cracknell, K. Latanoprost and pigmentation. Jpn. J. Ophthalmol. 48, 602-612 (2004).
26. Van Buskirk, E. M. Adverse reactions from timolol administration. Ophthalmology. 87, 447-450 (1980).
27. Sugrue, M. F. Pharmacological and ocular hypotensive properties of topical carbonic anhydrase inhibitors. Prog. Retin. Eye Res. 19, 87-112 (2000).
28. Garnock-Jones, K. P. Ripasudil: first global approval. Drugs 74, 2211-2215 (2014).
29. Isobe, T. et al. Effects of K-115, a rho-kinase inhibitor, on aqueous humor dynamics in rabbits. Curr. Eye Res. 39, 813-822 (2014).
30. Tanihara, H. et al. The K-115 Clinical Study Group. Intra-ocular pressure-lowering effects of a Rho kinase inhibitor, ripasudil (K-115), over 24 hours in primary open-angle glaucoma and ocular hypertension: A randomized, open-label, crossover study. Acta Ophthalmol. 93, e254-e260 (2015).
31. Tanihara, H. et al. K-115 Clinical Study Group. Phase 2 randomized clinical study of a Rho kinase inhibitor, K-115, in primary openangle glaucoma and ocular hypertension. Am. J. Ophthalmol. 156, 731-736 (2013).
32. Tanihara, H. et al. K-115 Clinical Study Group. Phase 1 clinical trials of a selective Rho kinase inhibitor, K-115. JAMA Ophthalmol. 131, 1288-1295 (2013).
33. Zamora, D. O. & Kiel, J. W. Topical proparacaine and episcleral venous pressure in the rabbit. Invest. Ophthalmol. Vis. Sci. 50, 2949-2952 (2009).
34. Tokushige, H. et al. Effects of topical administration of Y-39983, a selective rho-associated protein kinase inhibitor, on ocular tissues in rabbits and monkeys. Invest. Ophthalmol. Vis. Sci. 48, 3216-3222 (2007).
35. Van de Velde, S. et al. AMA0076, a novel, locally acting Rho kinase inhibitor, potently lowers intraocular pressure in New Zealand white rabbits with minimal hyperemia. Invest. Ophthalmol. Vis. Sci. 55, 1006-1016 (2014).
36. Lu, Z., Overby, D. R., Scott, P. A., Freddo, T. F. & Gong, H. The mechanism of increasing outflow facility by rho-kinase inhibition with Y-27632 in bovine eyes Exp. Eye Res. 86, 271-281 (2008).
37. Bill, A. Conventional and uveo-scleral drainage of aqueous humor in the cynomolgus monkey (Macaca irus) at normal and high intraocular pressures. Exp. Eye Res. 5, 45-54 (1966).
38. Pederson, J. E., Gaasterland, D. E. & MacLellan, H. M. Uveoscleral aqueous outflow in the rhesus monkey: importance of uveal reabsorption. Invest. Ophthalmol. Vis. Sci. 16, 1008-1017 (1977).
39. Tan, J. C., Peters, D. M. & Kaufman, P. L. Recent developments in understanding the pathophysiology of elevated intraocular pressure. Curr. Opin. Ophthalmol. 17, 168-174 (2006).
40. Grant, W. M. Experimental aqueous perfusion in enucleated human eyes. Arch. Ophthalmol. 69, 783-801 (1963).
41. Rosenquist, R., Epstein, D., Melamed, S., Johnson, M. & Grant, W. M. Outflow resistance of enucleated human eyes at two different perfusion pressures and different extents of trabeculotomy. Curr. Eye Res. 8, 1233-1240 (1989).
42. Johnson, M. What controls aqueous humor outflow resistance ? Exp. Eye Res. 82, 545-557 (2006).
43. Weinreb, R. N. & Khaw, P. T. Primary open-angle glaucoma. Lancet 363, 1711-1720 (2004).
44. Acott, T. S. & Kelley, M. J. Extracellular matrix in the trabecular meshwork. Exp. Eye Res. 86, 543-561 (2008).
45. Rao, V. P. & Epstein, D. L. Rho GTPase/Rho kinase inhibition as a novel target for the treatment of glaucoma. BioDrugs 21, 167-177 (2007).
46. Koga, T. et al. Rho-associated protein kinase inhibitor, Y-27632, induces alterations in adhesion, contraction and motility in cultured human trabecular meshwork cells. Exp. Eye Res. 82, 362-370 (2006).
47. Khuranaa, R. N., Denga, P.-F., Epstein, D. L. & Rao, V. P. The role of protein kinase C in modulation of aqueous humor outflow facility. Exp. Eye Res. 76, 39-47 (2003).
48. Kameda, T. et al. The effect of Rho associated protein kinase inhibitor on monkey Schlemm's canal endothelial cells. Invest. Ophthalmol. Vis. Sci. 53, 3092-3103 (2012).
49. Underwood, J. L. Glucocorticoids regulate transendothelial fluid flow resistance and formation of intercellular junctions. Am. J. Physiol. 277, C330-342 (1999).
50. Fujimoto, T. et al. Involvement of RhoA/Rho-associated kinase signal transduction pathway in dexamethasone-induced alterations in aqueous outflow. Invest. Ophthalmol. Vis. Sci. 53, 7097-7108 (2012).
51. Alvarado, J. A., Betanzos, A., Franse-Carman, L., Chen, J. & González-Mariscal, L. Endothelia of Schlemm's canal and trabecular meshwork: distinct molecular, functional, and anatomic features. Am. J. Physiol. Cell Physiol. 286, C621-634 (2004).
52. Underwood, J. L. et al. Glucocorticoids regulate transendothelial fluid flow resistance and formation of intercellular junctions. Am. J. Physiol. 277, C330-342 (1999).